2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. Pyruvate Kinase

Pyruvate Kinase

Pyruvate Kinase

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Pyruvate kinase is an enzyme that catalyzes the conversion of phosphoenolpyruvate and ADP to pyruvate and ATP in glycolysis and plays a role in regulating cell metabolism. There are four mammalian pyruvate kinase isoforms with unique tissue expression patterns and regulatory properties. Pyruvate kinase has four different tissue-specific isozymes in animals, PKL, PKR, PKM1, and PKM2. The L and R isozymes are expressed in the liver (L) and red blood cells (R), whereas PKM2 is expressed in early embryonic cells and other proliferating cells, and PKM1 is expressed in the brain, skeletal muscle, and heart which need high energy.

PKM1 and PKM2 are formed by a single mRNA transcript of the PKM gene by alternative splicing. The oligomers of PKM2 exist in high activity tetramer and low activity dimer forms. The dimer PKM2 regulates the rate-limiting step of glycolysis that shifts the glucose metabolism from the normal respiratory chain to lactate production in tumor cells. Besides its role as a metabolic regulator, it also acts as a protein kinase, which contributes to tumorigenesis. PKM2 serves as a promising target for cancer treatment.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-159095
    PKR activator 5
    		Activator
    PKR activator 5 (Compound 18) is an activator for pyruvate kinase R (PKR) with an AC50 of 28 nM.
    PKR activator 5
  • HY-155216
    PKM2 activator 10
    		Activator
    PKM2 activator 10 (Compd I) is a PKM2 activator with anti-tumor activity. PKM2 activator 10 can be utilized in cancer research.
    PKM2 activator 10
  • HY-W753956
    Iminostilbene-d10
    Iminostilbene-d10 is the deuterium labeled Iminostilbene (HY-N7064). Iminostilbene is a chemical precursor of carbamazepine. Additionally, Iminostilbene is an orally active inhibitor of PKM2 (Pyruvate Kinase M2) and COX2 (Cyclooxygenase-2). Iminostilbene exerts its effects by inhibiting PKM2 and its interaction with HIF-1α and STAT3, reducing COX2 and iNOS expression, and decreasing LPS-induced release of IL-1β, IL-6, TNF-α, and MCP-1, thereby suppressing macrophage-mediated inflammatory responses and improving myocardial ischemia/reperfusion (MI/R) injury. Iminostilbene holds promise for research in inflammation regulation, cardiovascular diseases (such as MI/R injury), and macrophage-mediated immune-related diseases.
    Iminostilbene-d<sub>10</sub>
  • HY-172881
    PKM2-IN-10
    		Inhibitor
    PKM2-IN-10 (Compound 16) is a PKM2 inhibitor. PKM2-IN-10 inhibits the proliferation of A549 and HCC1833 cell lines with IC50 of 3.36 μM and 9.20 μM, respectively. PKM2-IN-10 exhibits antitumor activity in human non-small cell lung cancer (NSCLC) and mouse lung adenocarcinoma models. PKM2-IN-10 can be used in lung cancer research.
    PKM2-IN-10
  • HY-168883
    PKM2 modulator 2
    		Inhibitor
    PKM2 modulator 2 (compound C599) is a potent PKM2 inhibitor. PKM2 modulator 2 shows antiproliferative activity. PKM2 modulator 2 induces apoptosis. PKM2 modulator 2 has the potential for the research of glioblastoma.
    PKM2 modulator 2
  • HY-E70953
    Pyruvate Kinase/Lactic Dehydrogenase enzymes, Rabbit
    Pyruvate Kinase/Lactic Dehydrogenase enzymes, Rabbit catalyzes an ATP-dependent phosphorylation of glycolate to yield 2-phosphoglycolate. Pyruvate kinase requires bivalent and monovalent cations such as Mg2+ and K+ respectively for activation to occur.
    Pyruvate Kinase/Lactic Dehydrogenase enzymes, Rabbit
  • HY-180523
    PKM2-IN-13
    		Inhibitor
    PKM2-IN-13 is a selective PKM2 inhibitor inhibiting PKM2 with an IC50 value of 55.13 μM. PKM2-IN-13 exhibits broad-spectrum anticancer activity with low toxicity to normal cells. PKM2-IN-13 induces apoptosis by elevated ROS levels and activation of caspases 3/7, and interacts with and inhibits the glycolytic activity of Pyruvate Kinase M2 in virto. PKM2-IN-13 demonstrates a favorable safety profile with no significant adverse effects in vivo. PKM2-IN-13 can be used for oral squamous cell carcinoma (OSCC), colon carcinoma, breast cancer and melanoma research.
    PKM2-IN-13
  • HY-178748
    PKM2-IN-12
    		Inhibitor
    PKM2-IN-12 is an orally active PKM2 inhibitor with an IC50 of 10 nM. PKM2-IN-12 inhibits COLO-205 cell proliferation and migration, arrests the cell cycle, and induces apoptosis. PKM2-IN-12 significantly reduces cellular levels of lactate, pyruvate, and ROS. PKM2-IN-12 directly kills cancer cells and restores disrupted gut microbiota balance in mice model. PKM2-IN-12 can be used to study colorectal cancer.
    PKM2-IN-12
  • HY-170577
    PKM2-IN-8
    		Inhibitor
    PKM2-IN-8 (Compound 9b) is a pyruvate kinase M2 (PKM2) inhibitor (IC50 = 0.31 μM). PKM2-IN-8 has potent antiproliferative activity against U87MG glioma cells. PKM2-IN-8 can induce early apoptosis and reduce lactate levels. PKM2-IN-8 can be used for the research of glioblastoma.
    PKM2-IN-8
  • HY-148313
    PKM2 activator 4
    		Activator
    PKM2 activator 4 is a PKM2 activator with an AC50 value of 1-10 μM. PKM2 activator 4 can be used for the research of cancer.
    PKM2 activator 4
  • HY-N7064R
    Iminostilbene (Standard)
    		Inhibitor
    Iminostilbene (Standard) is the analytical standard of Iminostilbene. This product is intended for research and analytical applications. Iminostilbene is a a chemical precursor of carbamazepine.
    Iminostilbene (Standard)
  • HY-168337
    SET-171
    		Inhibitor
    SET-171 is a JNK (c-Jun N-terminal kinase) inhibitor that exhibits significant anticancer activity and lipid metabolism regulation by inhibiting liver pyruvate kinase (PKL) expression. In anticancer studies, SET-171 shows IC50 values of 8.82 μM and 2.97 μM against HepG2 and Huh7 cell lines, respectively, indicating high cytotoxicity. Additionally, in non-alcoholic fatty liver disease (NAFLD)-related studies, SET-171 significantly reduces triacylglycerol (TAG) levels and inhibits the expression of steatosis-related proteins. SET-171 holds promise for research on hepatocellular carcinoma (HCC) and NAFLD.
    SET-171
  • HY-12689B
    Mitapivat hemisulfate
    		Activator
    Mitapivat hemisulfate is an orally active pyruvate kinase allosteric activator. Mitapivat hemisulfate increases enzymatic activity, protein stability, and ATP levels over a broad range of PKLR genotypes, shows the potential to restore the activity of PK (pyruvate kinase)-deficient glycolytic pathways. Mitapivat hemisulfate can be used in study of PK deficiency.
    Mitapivat hemisulfate
  • HY-12689A
    Mitapivat hemisulfate sesquihydrate
    		Activator
    Mitapivat hemisulfate sesquihydrate (AG-348) is an orally active pyruvate kinase allosteric activator. Mitapivat increases enzymatic activity, protein stability, and ATP levels over a broad range of PKLR genotypes, shows the potential to restore the activity of PK (pyruvate kinase)-deficient glycolytic pathways. Mitapivat can be used in study of PK deficiency.
    Mitapivat hemisulfate sesquihydrate
  • HY-D1877
    ZY-1
    		98.91%
    ZY-1 is a control molecule of ZY-2 (HY-D1876, a PKM2 fluorescent probe). ZY-1 shows a low fluorescence emission in HeLa, a cervical cancer cell abundant in PKM2 expression.
    ZY-1
  • HY-178441
    PKM2-IN-11
    		Inhibitor
    PKM2-IN-11 is a PKM2 inhibitor (IC50 = 0.363 μM). PKM2-IN-11 has dual mechanisms involving pyruvate kinase M2 (PKM2) inhibition and microtubule stabilization. PKM2-IN-11 can decrease PKM2 protein levels in MCF-7 cells. PKM2-IN-11 can slightly reduce reactive oxygen species (ROS) levels and significantly increase early apoptotic cells. PKM2-IN-11 induces G2/M phase arrest. PKM2-IN-11 can be used for the study of breast cancer.
    PKM2-IN-11
  • HY-12689C
    Mitapivat hydrochloride
    		Activator
    Mitapivat (AG-348) hydrochloride is an orally active and selective allosteric pyruvate kinase R (PK-R) activator. Mitapivat hydrochloride accelerates the reaction of PK-R catalyzing the conversion of phosphoenolpyruvate to pyruvate, thereby promoting the glycolytic pathway, increasing the production of adenosine triphosphate (ATP) in red blood cells, and reducing the level of 2,3-diphosphoglycerate (2,3-DPG). Mitapivat hydrochloride is promising for research of pyruvate kinase deficiency and other anemia-related diseases.
    Mitapivat hydrochloride
  • HY-P3201
    PKCζ/ι pseudosubstrate inhibitor
    		Inhibitor
    PKCζ/ι pseudosubstrate inhibitor has broad-spectrum effects on the PKC enzyme family and can induce memory impairment.
    PKCζ/ι pseudosubstrate inhibitor
  • HY-B1814
    Vitamin K5
    		Inhibitor
    Vitamin K5 (Synkamin) is a photosensitizer and a antimicrobial agent. Vitamin K5 is a specific PKM2 inhibitor with IC50 values of 28, 191 and 120 μM for PKM2, PKM1 and PKL. Vitamin K5 induces apoptosis of colon 26 cells. Vitamin K5 can be used for the research of infection and cancer, and it also can be used as a preservative for pharmaceuticals, foods, and beverages.
    Vitamin K5
  • HY-182037
    Multi-target kinase-IN-9
    		Inhibitor
    Multi-target kinase-IN-9 is a multi-target enzyme inhibitor with antiproliferative and antiangiogenic activities, and exhibits remarkable selectivity against hepatocellular carcinoma cells. By broadly binding to the active sites or ATP-binding regions of multiple key enzymes including DNA polymerase β, Pyruvate Kinase M2 (PKM2), Multi-target kinase-IN-9 comprehensively disrupts DNA repair and replication, glycolysis, chromatin dynamics and transcriptional programs, and blocks the self-renewal of cancer stem cells. Multi-target kinase-IN-9 induces genomic instability, lysosomal dysfunction and autophagic flux impairment, thereby triggering tumor cell death, effectively inhibiting tumor proliferation, invasion, metastasis and angiogenesis, and significantly reducing tumor volume in xenograft models. Multi-target kinase-IN-9 is applicable to hepatocellular carcinoma-related research.
    Multi-target kinase-IN-9
Cat. No. Product Name / Synonyms Application Reactivity